Tubulin Binding, Protein-Bound Conformation in Solution, and Antimitotic Cellular Profiling of Noscapine and Its Derivatives

被引：31

作者：

Bennani, Youssef L. ^{[1
]}

Gu, Wenxin ^{[1
]}

Canales, Angeles ^{[2
]}

Diaz, Fernando J. ^{[3
]}

Eustace, Brenda K. ^{[1
]}

Hoover, Russell R. ^{[1
]}

Jimenez-Barbero, Jesus ^{[3
]}

Nezami, Azin ^{[1
]}

Wang, Tiansheng ^{[1
]}

机构：

[1] Vertex Pharmaceut Inc, Cambridge, MA 02139 USA

[2] Univ Complutense Madrid, Fac Ciencias Quim, Dept Quim Organ 1, E-28040 Madrid, Spain

[3] Consejo Super Invest Cient, Ctr Invest Biol, Dept Phys Chem, Madrid 28040, Spain

来源：

JOURNAL OF MEDICINAL CHEMISTRY | 2012年 / 55卷 / 05期

关键词：

AGENTS; CELLS;

D O I：

10.1021/jm200848t

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Noscapine and its 7-hydroxy and 7-amino derivatives were characterized for their binding to tubulin. A solution NMR structure of these compounds bound to tubulin shows that noscapine and its 7-aniline derivative do not compete for the same binding site nor does its small molecule crystal structure match its tubulin-bound conformation. These compounds were also tested for their antiproliferative effects on a panel hepatocellular carcinoma cell lines.

引用

页码：1920 / 1925

页数：6

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